Dimethylformamide → 2-[1-(2-Fluorobenzyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]pyrido[4,3-d]pyrimidin-5(6H)-one

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Reaction Conditions

Reaction Steps

Under argon, 21 mg (0.522 mmol) of sodium hydride (60% suspension in mineral oil) were initially charged and washed repeatedly with hexane. Subsequently, dimethylformamide (0.18 ml) was added, and a solution of 158 mg (0.435 mmol) of the compound from example 46A in dimethylformamide (6.0 ml) was added to the suspension. The reaction mixture was stirred at 150° C. for two days, then diluted with acetonitrile at RT, then filtered, and the filtrate was concentrated. The residue was separated by means of preparative HPLC (eluent: acetonitrile-water with 0.1% formic acid gradient) and the product fractions were concentrated. This gave 31 mg (18% of theory) of the title compound in solid form.

Provenance & Evidence